查看更多>>摘要：Four undescribed sulfoxide-containing derivatives, sinkiangenoxides A and B, (2Z, 4E)-sinkiangenoxide C, and (2E, 4E)-sinkiangenoxide C (1?–?4), and one known compound, 1-(methylthio)propyl (E)-1-propenyl disulfide (5), were isolated from the resin of Ferula sinkiangensis. Their structures were determined based on spectroscopic methods, including IR, UV, HRESIMS, NMR, and CD analysis. Compounds 2?–?4 showed moderate cytotoxic activities against four human cancer cell lines with IC50 values ranging from 15.0 to 40.3?μM. Sinkiangenoxide B (2) was shown to induce apoptosis in HepG2 cells. In addition, compound 5 effectively attenuated lipopolysaccharide-induced nitric oxide release and TNF-α, IL-1β, IL-6, and IL-10 expression.
Juliana A. A. do ValeAna C. ZanattaGustavo C. BressanLeandro L. de Oliveira...
11页
查看更多>>摘要：Athenaea velutina is a promising Brazilian shrub with cytotoxic and antimigratory properties against cancer cells. However, the mechanism of induction of cancer cell death and the compounds involved remain unknown. To ascertain these bioactive compounds, bioassay-guided fractionation was performed, alongside the appropriate in vitro tests. A withanolide-rich fraction (FAv_5) from the dichloromethane extract increased cytotoxic activity by 1.5-fold (IC50?=?2.1?μg/mL). Fourteen withanolide steroids were tentatively identified for the first time for this species by mass spectrometry coupled to liquid chromatography (LC MS/MS), including withanolide A, aurelianolide A, and aurelianolide B. FAv_5 significantly decreased cell proliferation, migration, and invasion with a selectivity index greater than 8 for B16F10 cells. Furthermore, flow cytometry with annexin V fluorescein isothiocyanate/propidium iodide (V-FITC/PI) staining showedFAv_5 to promote cell cycle arrest at the G0/G1-phase as well as apoptotic cell death. Overall, these findings highlight A.?velutina as a source of withanolide-steroids that inhibit cancer cell proliferation through apoptosis and cell cycle blockade mechanisms. Details on the geographic distribution of A.?velutina and species conservation strategies have also been highlighted.
查看更多>>摘要：Quercetin, a flavonol, is a functional compound that is abundant in onions and is known to have antioxidant and anti-inflammatory effects. Quercetin and its glucoside are known to function as peroxisome proliferator-activated receptor (PPAR) ligands and showed high PPAR-α transactivation activity but little PPAR-γ transactivation activity in some reports. In this study, we demonstrated that an aqueous extract of a quercetin-rich onion cultivar increased transactivation activities not only of PPAR-α but also of PPAR-γ. We isolated (9S,12S,13S)-(10E)-9,12,13-trihydroxyoctadec-10-enoic acid (pinellic acid) obtained from the aqueous extract using PPAR-γ transactivation as an index. Furthermore, it was revealed that pinellic acid could transactivate PPAR-α. Our findings are the first report mentioned showing that trihydroxyoctadec-10-enoic acids showed PPAR-α/γ transactivation activities.
查看更多>>摘要：Equiseti herba has been traditionally indicated in bacterial diseases of the efferent urinary tract or bad healing wounds in many regions worldwide. Most of the plant material used for medical purposes comes from collections of wild growing plants. The European Pharmacopoeia requires that Equiseti herba should consist of a minimum of 95% Equisetum arvense and a maximum of 5% foreign ingredients. This includes Equisetum palustre, which is known for its potentially toxic alkaloid palustrine. However, both Equisetum species are quite common, look morphologically very similar, and share similar habitats, hence, are therefore often confused. Recently, several structurally related Equisetum alkaloids have been identified in E. palustre but not in E. arvense. We have established a hydrophilic interaction liquid chromatography HPLC-ESI-MS/MS method for the detection of these E. palustre-specific Equisetum alkaloids in orderto quantify the contamination of Equiseti herba (E. arvense) by E. palustre plant material. In a second, independent approach, the results of the HPLC-MS/MS analysis were confirmed by scanning electron microscopy, looking for the species-specific characteristics of the stoma apparatus of E. palustre. Thirty-four Equiseti herba products obtained from different pharmacies, drug stores, supermarkets, and web stores were analyzed. The majority of the products (26 out of 34) were Equisetum alkaloid positive, with contents ranging from 0.29?–?21.7?mg of Equisetum alkaloids/kg (d.?w.). In addition, the transfer of Equisetum alkaloids into tea infusions was investigated, demonstrating a 42 to 60% transfer rate for cold and hot water extraction of Equisetum alkaloid-contaminated Equiseti herba, respectively.
查看更多>>摘要：A new sesquiterpene, chlorantholide G (1), a new sesquiterpene dimer, elatiolactone (2), and 2 new diterpenes, elatiorlabdane B (3) and elatiorlabdane C (4), together with 51?known compounds, were isolated from the aerial parts of Chloranthus elatior. The new structures including their absolute configurations were mainly established by mass spectrometric, NMR, and electronic circular dichroism experiments. All isolated compounds were tested for their anti-hDHODH activity. (4S,6R)-4-hydroxy-6-isopropyl-3-methylcyclohex-2-enone (5) and (4S,5R,9S,10R)-8(17),12,14-labdatrien-18-oic acid (29) were the most active compounds with IC50 values of 18.7 and 30.7?μM, respectively.
查看更多>>摘要：Identification of novel anti-inflammatory strategies are needed to avoid the side effects associated with the currently available therapies. Use of anti-inflammatory herbal remedies is gaining attention. The purpose of the present investigation was to evaluate the pharmacological potential of the withanolide-rich root extracts of the medical plant Withania somnifera (L.) Dunal using in vivo and in vitro models of endotoxin-induced inflammation and oxidative stress. The pharmacological effects of W. somnifera root extracts were evaluated using a mouse model of endotoxin (lipopolysaccharide)-induced peritonitis and various relevant human cell lines. HPLC analysis of the W. somnifera root extracts identified the presence of various bioactive withanolides. In vivo challenge of mice with endotoxin resulted in the infiltration of various leukocytes, specifically neutrophils, along with monocytes and lymphocytes into the peritonealcavity. Importantly, prophylactic treatment with W. somnifera inhibited the migration of neutrophils, lymphocytes, and monocytes and decreased the release of interleukin-1β, TNF-α, and interleukin-6 cytokines into the peritoneal cavity as identified by ELISA. Liver (glutathione peroxidase, glutathione, glutathione disulfide, superoxide dismutase, malondialdehyde, myeloperoxidase) and peritoneal fluid (nitrite) biochemical analysis revealed the antioxidant profile of W. somnifera. Similarly, in human HepG2 cells, W. somnifera significantly modulated the antioxidant levels. In THP-1 cells, W. somnifera decreased the secretion of interleukin-6 and TNF-α. In HEK-Blue reporter cells, W. somnifera inhibited TNF-α-induced nuclear factor-κB/activator protein 1 transcriptional activity. Our findings suggest the pharmacological effects of root extracts of W. somnifera rich in withanolidesinhibit neutrophil infiltration, oxidative hepatic damage, and cytokine secretion via modulating the nuclear factor-κB/activator protein 1 pathway.
Sandra Alves de Sousa GarciaPriscila Bianca Rodrigues da RochaBruno dos Santos SouzaAndressa Tuane Santana Paz...
10页
查看更多>>摘要：Punicalagin, the principal ellagitannin of Lafoensia pacari leaves, has proven antioxidant activity, and standardized extracts of L.?pacari can be topically used for skin aging management. We hypothesized that Pluronic nanomicelles or vesicles could solubilize sufficiently large amounts of the standardized extracts of L.?pacari and provide chemical stability to punicalagin. The standardized extracts of L.?pacari were obtained with an optimized extraction procedure, and the antioxidant activity was characterized. Formulations containing Pluronic at 25% and 35% were obtained with or without Span 80. They were characterized by average diameter, polydispersity index, punicalagin content, physicochemical stability, and rheology. A release and skin permeation study was carried out in vertical diffusion cells. The extraction procedure allowed quantifying high punicalagin content (i.e., 141.61?±?3.87?mg/g). The standardized extracts ofL.?pacari showed antioxidant activity for all evaluated methods. Pluronic at 25 and Pluronic at 35 with standardized extracts of L.?pacari showed an average diameter of about 25?nm. The addition of Span 80 significantly increased the mean diameter by 15-fold (p?<?0.05), indicating the spontaneous formation of vesicles. Pluronic formulations significantly protected punicalagin from chemical degradation (p?<?0.05). Pluronic at 25 formulations presented as free-flowing liquid-like systems, while Pluronic at 35 resulted in an increase of about 44-fold in |?*|. The addition of Span 80 significantly reduced the Pluronic sol-gel transition temperature (p?<?0.05), indicating the formation of vesicles. Formulations with Span 80 significantly enhanced punicalagin skin permeation compared to formulations without Span 80 (p?<?0.05). Formulations with Span 80 were demonstrated to be the most promising formulations, as they allowed significant permeation ofpunicalagin (about 80 to 315?μg/cm2), which has been shown to have antioxidant activity.
NSTL
Thieme Medical Publishers